| Reaction Details |
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 | Report a problem with these data |
| Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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| Ligand | BDBM124444 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1460217 (CHEMBL3369681) |
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| IC50 | 0.100000±n/a nM |
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| Citation |  Hu, E; Chen, N; Bourbeau, MP; Harrington, PE; Biswas, K; Kunz, RK; Andrews, KL; Chmait, S; Zhao, X; Davis, C; Ma, J; Shi, J; Lester-Zeiner, D; Danao, J; Able, J; Cueva, M; Talreja, S; Kornecook, T; Chen, H; Porter, A; Hungate, R; Treanor, J; Allen, JR Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A). J Med Chem57:6632-41 (2014) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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| Name: | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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| Synonyms: | 3',5'-cyclic phosphodiesterase | 3.1.4.17 | PDE10A | PDE10_HUMAN | Phosphodiesterase 10 (PDE10) | Phosphodiesterase 10A |
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| Type: | Protein |
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| Mol. Mass.: | 88412.52 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q9Y233 |
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| Residue: | 1055 |
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| Sequence: | MASLEEPLAPRPQGPLPAAGDEPGCGPGKLRPEPRLSAAGGGSAAGPGPAPEWPGRGRAE
RAAPPRPPLSSAGRPSPAGGPGALSARGGGCGWVAARAPLALAFSSRVPSSSPSFFYFWP
PPPPPPPSFLPSSSAFHLPVRLPGREGAAAAAAAGGGGDAGGGGGGGQEAAPLSVPTSSS
HRGGGGSGGGRRRLFLSPALQGLLLPARAGPRPPPPPRLPLGQAARRAGSPGFPGAGPGG
GGQTPRRPQGASFALAAAAALLFGSDMEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLS
LHPQVLDEFVSESVSAETVEKWLKRKNNKSEDESAPKEVSRYQDTNMQGVVYELNSYIEQ
RLDTGGDNQLLLYELSSIIKIATKADGFALYFLGECNNSLCIFTPPGIKEGKPRLIPAGP
ITQGTTVSAYVAKSRKTLLVEDILGDERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGIL
ELYRHWGKEAFCLSHQEVATANLAWASVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNI
VAIDSLLEHIMIYAKNLVNADRCALFQVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRF
SIEKGIAGQVARTGEVLNIPDAYADPRFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQM
VNKISGSAFSKTDENNFKMFAVFCALALHCANMYHRIRHSECIYRVTMEKLSYHSICTSE
EWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFIMS
VKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLCHDLDHRGFSNSY
LQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATD
LALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYA
EFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKA
CRDNLSQWEKVIRGEETATWISSPSVAQKAAASED
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| BDBM124444 |
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| n/a |
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| Name | BDBM124444 |
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| Synonyms: | US8759532, 99 |
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| Type | Small organic molecule |
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| Emp. Form. | C24H21N3O3 |
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| Mol. Mass. | 399.4418 |
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| SMILES | O=C(c1nc2ccccc2[nH]1)c1ccc(Oc2ncccc2C2CCOCC2)cc1 |
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| Structure | 
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